Gefitinib-based PROTAC 3
Cat. No.：YN340098
| 产品名称: | Gefitinib-based PROTAC 3 |
| CAS No.: | 2230821-27-7 |
| Chemical Name: | (2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)pentyl)oxy)ethoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Synonyms: | |
| 分子量: | 934.51 |
| 分子式: | C₄₇H₅₇ClFN₇O₈S |
| SMILES: | O=C([C@H]1N(C([C@@H](NC(CCOCCOCCCCCOC2=CC3=C(NC4=CC=C(F)C(Cl)=C4)N=CN=C3C=C2OC)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Gefitinib-based PROTAC 3，通过 linker 将 EGFR 结合元件与 VHL 配体结合，作用于 HCC827 (外显子 19 缺失) 和 H3255 (L858R 突变) 细胞，诱导EGFR降解，DC50分别为 11.7 nM 和 22.3 nM。 |
| IC50和靶点: | [{name:"EGFR:11.7 nM (DC50, HCC827(exon 19 del) cells)"},{name: "EGFR:22.3 nM (DC50, H3255 (L858R mutantion) cells)'}, 'PROTAC'] |
| In Vitro: | |
| In Vivo: | |
| Clinical Trial: | |
| Solvent & Solubility: |
Burslem, G.M., Smith, B.E., Lai, A.C., et al.The advantages of targeted protein degradation over inhibition: An RTK case studyCell Chem. Biol.25(1),66-77(2018)
